Drug intelligence / Profile preview

cyclophosphamide + methotrexate + N-(phosphonacetyl)-L-aspartate + sulfamethoxazole + pyrimethamine

Development stage
Preclinical
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Intravenous, Topical
01

Overview

This is a **non-standard combination drug** consisting of five agents: - **Cyclophosphamide**: An alkylating agent used as chemotherapy and immunosuppressant. - **Methotrexate**: A folic acid antagonist and antimetabolite, used in cancer and autoimmune disorders. - **N-(phosphonacetyl)-L-aspartate (PALA)**: A synthetic antimetabolite inhibiting de novo pyrimidine synthesis, active against solid tumors and showing immune modulatory effects via NOD2 activation[2][4][8][10]. - **Sulfamethoxazole**: A sulfonamide antibiotic, inhibits bacterial folic acid synthesis[3]. - **Pyrimethamine**: An antiparasitic and antifolate agent, primarily targeting protozoa. The mechanisms involve inhibition of DNA synthesis (by alkylation and anti-folate action), immunomodulation, and antimicrobial activity. This combination is not a recognized or marketed regimen but could be theoretically constructed for investigational use, targeting cancer, infections, or immune modulation.

Brand names
BactrimSeptraSulfatrim
Other names
cyclophosphamide + methotrexate + N-(phosphonacetyl)-L-aspartate + sulfamethoxazole + pyrimethamineco-trimoxazole
02

Targets

DHFR (Dihydrofolate reductase)CAD (Carbamoyl-phosphate synthetase 2, aspartate transcarbamoylase, and dihydroorotase)DHPS (Dihydropteroate synthase)DNA

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